Chitosan nanoparticles as a new delivery system for the chemotherapy agent tegafur

Background: Despite the very efficient antitumor activity of conventional chemotherapy, generally high doses of anticancer molecules must be administered to obtain the required therapeutic action, simultaneously leading to severe side effects. This is frequently a consequence of the development of multidrug resistance by cancer cells and of the poor pharmacokinetic profile of these agents. Objective: In Order to improve the antitumor effect of tegafur and overcome their important drawbacks, we have investigated its incorporation into a drug nanoplatform based on the biodegradable polymer chitosan. Materials and Methods: Two tegafur loading methods were studied: (i) absorption into the polymeric network (entrapment procedure); and (ii) surface deposition (adsorption procedure) in already formed chitosan nanoparticles. Results: Tegafur entrapment into the polymeric matrix has yielded higher drug loading values and a slower drug release profile, compared to single surface adsorption. The main factores determining the drug loading to chitosan were identified. Discussion and Conclusion: Such polymeric colloid present very interesting properties for efficient tegafur delivery to cancer.